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1357389-11-7

中文名称 RGFP966
英文名称 RGFP-966
CAS 1357389-11-7
分子式 C21H19FN4O
分子量 362.4
MOL 文件 1357389-11-7.mol
更新日期 2024/10/28 15:31:46
1357389-11-7 结构式 1357389-11-7 结构式

基本信息

中文别名
HDAC3抑制剂(RGFP966)
(2E)-N-(2-氨基-4-氟苯基)-3-[1-(3-苯基-2-丙烯-1-基)-1H-吡唑-4-基]-2-丙烯酰胺
英文别名
CS-871
RGFP966
RGFP-966
RGFP 966
(E/Z)-RGFP 966
RGFP966, >=98%
RGFP966
RGFP-966
(2E)-N-(2-Amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-2-propenamide
2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-, (2E)-
所属类别
生物化工:激动剂抑制剂

物理化学性质

沸点630.4±55.0 °C(Predicted)
密度1.19±0.1 g/cm3(Predicted)
储存条件-20°C
溶解度可溶于 DMSO(高达 20 mg/ml)
酸度系数(pKa)11.58±0.70(Predicted)
形态固体
颜色米白色
稳定性可在-20°C下的DMSO溶液保存长达1个月。
RGFP966价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/08/19HY-13909RGFP966
RGFP966
1357389-11-75mg900元
2024/08/19HY-13909RGFP966
RGFP966
1357389-11-710mM * 1mLin DMSO990元
2024/08/19HY-13909RGFP966
RGFP966
1357389-11-710mg1183元

常见问题列表

生物活性
RGFP966 是高选择性的 HDAC3 抑制剂,IC50 为 80 nM,在 15 μM 时对其他 HDAC 无抑制作用。RGFP966 能够透过血脑屏障 (BBB)。
靶点

HDAC3

80 nM (IC 50 )

体外研究

RGFP966 potently and selectively inhibits HDAC 3 with IC 50 of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC 50 =5.6 μM), 2 (9.7 μM) and 8 (>100 μM), indicating a good level of selectivity for HDAC 3. The mRNA levels of HDACs 1, 2 and 3 are not significantly affected by RGFP966 in RAW 264.7 macrophages, whereas the HDAC 1 and HDAC 2 protein levels are slightly, though significantly, reduced upon RGFP966 treatment. Moreover, RGFP966 significantly reduced the transcriptional activity of NF-κB p65, whereas NF-κB p65 acetylation and localization remain unaltered.

体内研究

RGFP966 (10 and 25 mg/kg) treatment significantly improves body weight, rotarod performance and several measures of motor function in the open field locomoter test. RGFP966 at a 10 mg/kg dose penetrates the blood-brain barrier into rat auditory cortex with typical pharmacokinetics, which together establish feasibility for the modulation of A1 plasticity due to action in the auditory cortex.

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